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Y 11

Cat. No. M7497
Y 11 Structure
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Biological Activity

Y 11 is a potent inhibitor of focal adhesion kinase (FAK); prevents FAK autophosphorylation at the Y397 site (IC50 ~ 50 nM in an in vitro kinase assay). Displays selectivity for FAK over a panel of other kinases (concentration used in assay = 1 μM). Decreases cell viability in a number of cancer cell lines; blocks colony formation in SW620 and BT474 cell lines.

Chemical Information
Molecular Weight 265.15
Formula C8H17N4OBr
CAS Number 1086639-59-9
Solubility (25°C) Water 26.52 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kim, et al. J Steroid Biochem Mol Biol. Evaluation of RU28318 and RU40555 as selective mineralocorticoid receptor and glucocorticoid receptor antagonists, respectively: receptor measures and functional studies.

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